Progress in Medicinal Chemistry 

About: Progress in Medicinal Chemistry is an academic journal published by Elsevier BV. The journal publishes majorly in the area(s): Receptor & Histamine. It has an ISSN identifier of 0079-6468. Over the lifetime, 344 publications have been published receiving 12659 citations.

Antimicrobial activity and action of silver

Abstract: Publisher Summary This chapter discusses antimicrobial activity and action of silver. Silver and its compounds have long been used, in one form or another, as antimicrobial agents. The silver compound of major therapeutic interest at the present time is silver sulphadiazine. Many in healthcare know that other silver compounds are still in use. It is worth stating that the treatment of ophthalmia neonatorum was revolutionized by the instillation of silver derivatives into the eyes of new-born sufferers. Several factors influence the antimicrobial activity of silver salts. Silver has a marked tendency to adsorb to surfaces and bactericidal activity is reduced in the presence of phosphates, chlorides, sulphides and hard water. Activity is increased as the temperature is raised and is pH-dependent, increasing with increasing pH. Sodium thioglycollate has been recommended as a suitable neutralizing agent for use in bactericidal testing although other SH compounds also fulfil this role. Silver, one of the native metals and second only to gold in its stability amongst the metals of antiquity, has provided several therapeutic agents which have been employed since the beginning of recorded history. These agents range from the metal itself, its salts and complexes with proteins and other macromolecules to the latest, silver sulphadiazine (AgSD).

Fluorine in medicinal chemistry.

Abstract: Since its first use in the steroid field in the late 1950s, the use of fluorine in medicinal chemistry has become commonplace, with the small electronegative fluorine atom being a key part of the medicinal chemist's repertoire of substitutions used to modulate all aspects of molecular properties including potency, physical chemistry and pharmacokinetics. This review will highlight the special nature of fluorine, drawing from a survey of marketed fluorinated pharmaceuticals and the medicinal chemistry literature, to illustrate key concepts exploited by medicinal chemists in their attempts to optimize drug molecules. Some of the potential pitfalls in the use of fluorine will also be highlighted.

Copper complexes offer a physiological approach to treatment of chronic diseases.

Abstract: Publisher Summary This chapter discusses copper complexes that offer a physiological approach to the treatment of chronic diseases. Copper is recognized as an essential metalloelement just as sodium, potassium, magnesium, calcium, iron, zinc, chromium, vanadium, and manganese. Just as essential amino acids, essential fatty acids and essential cofactors (vitamins), essential metalloelements are required for normal metabolic processes but cannot be synthesized de novo, and daily dietary intake and absorption are required. The adult body contains between 1.4 mg (22 pmol) and 2.1 mg (33 pmol) of copper per kilogram of body weight while the infant body contains three times this amount, consistent with the fact that infant metabolic needs are that much greater than those of adults. The essentiality of copper is now understood as being based upon its recognized need for activation of copper-dependent enzymes. Complexed forms of copper also facilitate absorption, tissue distribution, and tissue utilization. In the nondisease state, these forms of copper account for the physiologic regulation of copper-dependent homeostatic processes. Consistent with the newly found role for copper in synthesis of neuroendocrine peptides, the copper complex of histidine has been found to increase the secretion of luteinizing hormone-releasing hormone (LH-RH) from granules of the median eminence.

Medicinal chemistry of tetrazoles.

Abstract: Publisher Summary Tetrazole itself exhibits no pharmacological activity; however, many of its derivatives possess interesting biological actions. The tetrazole function is metabolically stable and this feature and a close similarity between the acidic character of the tetrazole group and the carboxylic group have inspired syntheses of potential medicinal agents. This chapter discusses the literature on the medicinal chemistry of tetrazoles. The most successful drug among the CNS acting tetrazole derivatives has been leptazol. The tetrazole system is metabolically stable and it may be of interest to introduce this stable lump on biologically active moieties and examine the effect produced on the activity. There are several instances of introduction of tetrazole heterocycle in the synthesis of new medicinal agents. A particular mention has been made of the promising anti-bacterial cephalosporin derivatives cephazolin sodium, ceftezole, and cephamandole.

Amidines and guanidines in medicinal chemistry.

Abstract: Publisher Summary This chapter focuses on amidines and guanidines in medicinal chemistry. The drugs are classified under their main physiological activities and within each group are arranged roughly in order of increasing molecular complexity. Many of the compounds have given temporary excitement to their discoverers and then been dropped—the commonest experience in medicinal chemistry. There are important, clinically used, medicines in all the major categories of therapeutic action discussed in the chapter. This simple and very unstable compound is not only a neurotransmitter in the brain, but acts in the dilation of blood vessels and activates leucocytes to attack tumour cells, fungi, and bacteria. In addition, nitric oxide can inhibit blood coagulation by preventing platelet aggregation and appears to be the regulator of the male erection. No doubt other functions will be discovered in the future, but the interesting finding for the present chapter is that the NO is formed by nitric oxide synthetase from arginine—the only essential amino acid which carries a guanidine group. Since most of the active guanidine drugs have at least one unsubstituted =NH or NH 2 group, it is interesting to speculate that they will be shown to act by giving nitric oxide as well.